Joint pain, swelling and deformity are relatively common complaints in elderly patients. These symptoms are usually caused by the deterioration of the joint cartilage that occurs with age, and/or by conditions associated with inflammation, trauma or reduced synovial liquid in the joints. Pain is frequently severe and requires administration of drugs with anti-inflammatory properties but which also have important adverse effects (gastritis, cardiovascular events, etc.) that occur especially with the extended use needed to treat these chronic articular ailments. Such drugs may include analgesics (painkillers) (such as acetaminophens and modified opioids), and NSAIDs (non-steroidal anti-inflammatory drugs), such as COX-1 and COX-2 inhibitors (e.g., Alevia, Celebrex, etc.). Other treatments used for alleviating the pain include steroids which may be delivered orally or intra-articularly (e.g. Prednisone, Hyalgan, Synvisc, etc), monoclonal antibodies which block molecules associated with the inflammatory response (e.g., Enbrel), and surgery (both classic and endoscopic) to extricate damaged cartilage and in severe cases to replace the affected joint.
Utilization of drugs in the form of topical ointments mitigates the adverse effects, but is usually regarded as less effective due to limited availability of the active substance in the affected tissue. While topical ointments may have reduced adverse effects, they still present the same drug safety profiles (they cause similar adverse effects).
The drugs and treatments used for decreasing pain may cause adverse side effects of different severity and health manifestations: some obvious (gastritis, gastro-esophageal reflux, gastric ulcer, etc.) and some more insidious (cardiovascular deterioration with increased risk for cardiovascular events).
Natural extracts from various plants have been used traditionally. Plant extracts are generally regarded as having less side effects but also as being less effective than drugs.
Commonly used extracts used with some success and mostly as individual extracts for relieving pain and symptoms associated with degenerative joint diseases include extracts of Juniperus, Helleborus, Tamus, Salix, Pinus. These extracts are mixed with a base made of mineral fats (e.g., paraffin) or other fatty substances with non-vegetal origin (lanolin, beeswax), or animal fat. In order to maintain high miscibility of the plant extracts with the base, emulsifiers, correctors, and preservatives are used.
The miscibility of plant extracts with mineral fats or non-vegetal fatty substances is low. Thus, emulsifiers are required in such mixtures, to keep the plant extracts evenly dispersed in the base. Adding an emulsifier or preservative as a specialized substance increases the possibility of allergic and other adverse reactions (one such example is the recent banning of parabens use in Europe), and increases the number of ingredients and manufacturing costs without adding therapeutic benefits.
The plant (vegetal) fats contains ample amounts of fatty acids which have been by themselves used successfully to treat arthritis and joint pain; one such example is a mixture of mainly long-chained, saturated fatty acids (stearic, linoleic, myristic, etc.) which are available to be administered both systemically (tablets) or topically (cream). However the former form increases the risk for developing insulin resistance, prediabetes and diabetes, while the latter is not as efficacious because of the low bioavailability (crossing of skin). Our composition overcomes this problem and adds to the benefits of fatty acids for treating articular problems.
Moreover, the composition bases used in the prior art have a substantial hydric content. Such bases need additional types and amounts of preservatives, mineral fats or non-vegetal to keep the plant extracts evenly dispersed in the base.
For example, a composition made in the Russian Federation for veterinarian use includes a specific, patented mix of plant extracts (Eucalyptus, Cedrus brevifolia, Pinus sibirica, Syzygium aromaticum, Lavandula angustifolia, Rosmarinus officinalis, Potentilla erecta, Juniperus communis, Myrtus communis, Vaccinium oxycoccos, Aesculus hippocastanum, Inula helenium, camphor, menthol cayenne, turpentine), along with dimethylsulfoxide, glycerin, methylchloroiso-thiasolinone, methylisothiasolinone. However the base of this prior art composition is a synthetic hidrophylic substance (polidone and carbopole in water, which together with chitosan make up more than 70% of the ointment by mass.